Salt forms of fatty acids for the treatment of dry eye

Abstract

Provided herein are compositions for the treatment of dry eye, comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a fatty acid salt, and methods of use thereof.

1 . A composition for the treatment of dry eye comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a fatty acid salt of Formula I: 
       
         
           
           
               
               
           
         
       
       a fatty acid salt of Formula II: 
       
         
           
           
               
               
           
         
       
       a fatty acid salt of Formula III: 
       
         
           
           
               
               
           
         
       
       a fatty acid salt of Formula IV: 
       
         
           
           
               
               
           
         
       
       a fatty acid salt of Formula V: 
       
         
           
           
               
               
           
         
       
       a fatty acid salt of Formula VI: 
       
         
           
           
               
               
           
         
       
       a fatty acid salt of Formula VII: 
       
         
           
           
               
               
           
         
       
       or a fatty acid salt of Formula VIII: 
       
         
           
           
               
               
           
         
         wherein FA −  is an anion of an omega-3 or omega-6 polyunsaturated fatty acid, and X −  is an anion of a pharmaceutically acceptable acid compound, or a combination thereof. 
       
     
     
         2 . The composition of  claim 1 , wherein the fatty acid salt is a compound of Formula I, Formula II, or Formula III. 
     
     
         3 . The composition of  claim 1  wherein FA −  is an anion of an omega-3 fatty acid, and the omega-3 fatty acid is selected from the group consisting of alpha-linolenic acid, stearidonic acid, eicosapentaenoic acid, and docosahexaenoic acid. 
     
     
         4 . The composition of  claim 1 , wherein FA −  is an anion of an omega-3 fatty acid, and the omega-3 fatty acid is eicosapentaenoic acid or docosahexaenoic acid. 
     
     
         5 . The composition of  claim 1 , wherein FA −  is an anion of an omega-6 fatty acid, and the omega-6 fatty acid is selected from the group consisting of linoleic acid, gammalinolenic acid, dihomogammalinoleic acid, and arachidonic acid. 
     
     
         6 . The composition of  claim 1 , formulated for topical administration to the eye of the subject in need thereof. 
     
     
         7 . The composition of  claim 6 , further comprising one or more of glycerin, hypromellose, propylene glycol or polyethylene glycol. 
     
     
         8 . The composition of  claim 6 , further comprising one or more of polysorbate 80, carbomer copolymer type A, purified water, sodium hydroxide, ascorbic acid, benzalkonium chloride, boric acid, dextrose, disodium phosphate, glycine, magnesium chloride, potassium chloride, sodium borate, sodium chloride, sodium citrate, sodium lactate, edetate disodium, hydrochloric acid, sodium hydroxide, aminomethylpropanol, hydroxypropyl guar, polyquaternium-1, or sorbitol. 
     
     
         9 . A method for the treatment of dry eye in a subject in need thereof, comprising administering to the subject the composition of  claim 1 . 
     
     
         10 . The method of  claim 9 , wherein dry eye is selected from the group consisting of alacrima, xerophthalmia, Sjogren's syndrome associated dry eye, non-Sjogren's syndrome associated dry eye, dry keratoconjunctivitis, ocular pemphigoid, dry eye after ophthalmic operation, and dry eye accompanied with conjunctivitis. 
     
     
         11 . The method of  claim 9 , wherein dry eye is aqueous tear-deficient dry eye or evaporative dry eye. 
     
     
         12 . A method for increasing tear production in a subject comprising administering to the subject the composition of  claim 1 . 
     
     
         13 . A method for the treatment of corneal ulceration, uveitis, or corneal transplant rejection in a subject, comprising administering to the subject the composition of  claim 1 . 
     
     
         14 . The method of  claim 9 , wherein the composition is applied topically to the eye of the subject.